Genistein

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Genistein

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

446-72-0

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
100mg	电议

产品介绍

化学性质

Storage	Store at -20°C
M.Wt	270.24
Cas No.	446-72-0
Formula	C₁₅H₁₀O₅
Solubility	≥13.5 mg/mL in DMSO; insoluble in H2O; ≥2.59 mg/mL in EtOH with gentle warming
Chemical Name	5,7-dihydroxy-3-(4-hydroxyphenyl)chromen-4-one
Canonical SMILES	C1=CC(=CC=C1C2=COC3=CC(=CC(=C3C2=O)O)O)O
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Genistein is a highly specific inhibitor of tyrosine kinase with IC50 value of ~ 8 μM [1].

Tyrosine protein kinase activities are known to be associated with oncogene products of the retroviral “src” gene family and with various cellular growth factor receptors including epidermal growth factor (EGF), platelet derived growth factor (PDGF), insulin and insulin-like growth factors, which play a key role in tumorogenesis. Thus, inhibitors of protein tyrosine kinase activity might represent a new class of antitumor agents [2].

In NIH-3T3 cells, Genistein blocked the mitogenic effect mediated by EGF with IC50 value of 12 μM or by insulin with IC50 value of 19 μM. In NIH-3T3 cells treated with EGF, Genistein partially prevented the increase of S6 kinase activity at 6 μM, with the maximal effect observed at 15 μM [2].

In a chemically (N-methylnitrosourea) induced prostate cancer rat model, Genistein (0, 25 or 250 mg/kg, p.o.) in the diet dose-dependently inhibited the development of invasive adenocarcinomas. In a transgenic mouse model that spontaneously developed prostate cancer, Genistein (0, 100, 250 or 500 mg/kg, p.o.) in the diet lowered the incidence of poorly differentiated prostatic adenocarcinomas in a dose-dependent manner [3].

References:

[1]. Baltuch G H, Yong V W. Signal transduction for proliferation of glioma cells in vitro occurs predominantly through a protein kinase C-mediated pathway. Brain Research, 1996, 710(1-2): 143-149.

[2]. Linassier C, Pierre M, Le Pecq J B, et al. Mechanisms of action in NIH-3T3 cells of genistein, an inhibitor of EGF receptor tyrosine kinase activity. Biochemical Pharmacology, 1990, 39(1): 187-193.

[3]. Lamartiniere C A, Cotroneo M S, Fritz W A, et al. Genistein chemoprevention: timing and mechanisms of action in murine mammary and prostate. Journal of Nutrition, 2002, 132(3): 552S-558S.

试验操作

细胞实验 [1]:
细胞系	NIH-3T3细胞
制备方法	在DMSO中的溶解度大于55.6 mg/mL。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。
反应条件	0 ~ 1000 μM
实验结果	给予4 ~ 75 μM Genistein，72小时后，NIH-3T3细胞生长受抑制。在浓度低于40 μM时，经过Genistein处理的细胞于停药后恢复生长。相比之下，在浓度等于或高于75 μM时，经过Genistein处理的细胞不能恢复生长。给予Genistein，3小时后，通过测定克隆效率来评估细胞毒性，其ED50值为35 μM。
动物实验 [2]:
动物模型	雌性SD大鼠
给药剂量	0、25和250 mg Genistein/kg AIN-76A；口服给药
实验结果	在雌性SD大鼠中，Genistein呈剂量依赖性地抑制二甲基苯并[a]蒽 (DMBA) 诱导的乳腺肿瘤发展。经过25和250 mg Genistein/kg AIN-76A处理的大鼠分别显示出7.1和4.3个乳腺肿瘤。Genistein通过调节特定的性类固醇受体以及生长因子信号通路来抑制乳腺肿瘤发展。
注意事项	请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。
References: [1]. Linassier C, Pierre M, Le Pecq JB, Pierre J. Mechanisms of action in NIH-3T3 cells of genistein, an inhibitor of EGF receptor tyrosine kinase activity. Biochem Pharmacol. 1990 Jan 1;39(1):187-93. [2]. Lamartiniere CA, Cotroneo MS, Fritz WA, Wang J, Mentor-Marcel R, Elgavish A. Genistein chemoprevention: timing and mechanisms of action in murine mammary and prostate. J Nutr. 2002 Mar;132(3):552S-558S.